PBA-RDPA 2013 Bologna, 30 June 3 July 2013

P1-69

CYTOTOXIC PRINCIPLES FROM EUPHORBIA NERIIFOLIA EXTRACT


L.-C. Lin
1
, Y.-J. Chen
2
, T.-H. Tsai
3

1
National Research Institute of Chinese Medicine, Taipei, Taiwan
2
Department of Radiation Oncology, Mackay Memorial Hospital, Taipei, Taiwan

3
Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei, Taiwan


Euphorbia neriifolia Linn. widely cultivated in tropical Asia, is a small deciduous tree of the family
Euphorbiaceae. The stems and leaves of E. neriifolia have been used traditionally with therapeutically
purposes for treatment of liver, uterine, breast, gastric and colon cancers in Formosa folk medicines. Our
preliminary bioassay also showed that the ethanolic extract of E. neriifolia possessed cytotoxic activities
against a small panel of human cancer lines. Although people had a lot of experiences on the use of E.
neriifolia, the active component for anticancer of E. neriifolia still remains unclear. The present study
aims at exploring the active compound of E. neriifolia extract on anticancer. Chromatography separation
of the ethyl acetate extract, an active extract of the aerial parts of E. neriifolia, has led to the isolation of
four triterpenoids [3 beta-Friedelinol (22), 3 alpha-Taraxerol (23), 3 beta-Taraxerol(24), 3 alpha-
Friedelinol (25)], and four lingols [3,7,12-O-triacetyl-8-O-tigloylingol (26), 3,7,12-O-triacetyl-8-O-
benzoylingol (27), 3,12-O-diacetyl-7-O-angeloyl-8-methoxyingol (28), and 3,12-O-diacetyl-8-methoxy-7-
O-benzoylingol (29)], together with known flavonoids, lignans, and phytosterols. Two pairs of isomers
22/25 and 23/24 can be separated using silica gel column in CHCl
3
eluent. The cytotoxic effects of these
isolated compounds were evaluated by MTT assay performing on human cancer cell lines of K562,
Panc-1, 81T, and BE3. 3 beta-Friedelinol (22), 3 beta-Taraxerol (24), 3 alpha-Friedelinol (25) showed
potent cytotoxic activity on Panc-1, 81T, and BE3 cancer lines, each compound with about 60% inhibition
rate at a concentration of 10 micromolar. 3 beta-Friedelinol (22), 3,7,12-O-triacetyl-8-O-tigloylingol (26)
and 3,12-O-diacetyl-7-O-angeloyl-8-methoxyingol (28) showed cytotoxic activities on K562 cell line, with
about 45%, 42%, and 53% inhibition rate at a concentration of 10 micromolar, respectively.

R
R
O
OCH
3
O
O
O
H
H
O
O
28
O
O
23 R= OH
24 R= OH
25 R= OH
22 R= OH